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Antibacterial and antibiofilm activities of synthetic analogs of 3-alkylpyridine marine alkaloids

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Nowadays, the emergence of superbugs is one of the most serious public health problems. Strains of Staphylococcus aureus and Klebsiella pneumoniae , resistant to many antimicrobials available in clinical practice,… Click to show full abstract

Nowadays, the emergence of superbugs is one of the most serious public health problems. Strains of Staphylococcus aureus and Klebsiella pneumoniae , resistant to many antimicrobials available in clinical practice, have become increasingly common. The development of new drugs for the treatment of infections caused by these pathogens is necessary and urgent. A series of 11 analogs of marine 3-alkylpyridine alkaloids was evaluated in vitro for its antibacterial potential. Compound 6 , a synthetic analog of viscosaline, exhibited significant activity against S. aureus , including an MRSA strain (MIC = 2 µg/mL). Additionally, it exhibited a 25% reduction in mature biofilm and a good selectivity index (SI > 16). None of the compounds exhibited activity against K. pneumoniae , but analog 6 was able to act in planktonic cells in the presence of polymyxin B at sub-inhibitory concentration. Compound 6 has promising anti-staphylococcal activity and future assays are encouraged to investigate their therapeutic potential.

Keywords: synthetic analogs; antibacterial antibiofilm; activities synthetic; analogs alkylpyridine; antibiofilm activities; alkylpyridine marine

Journal Title: Medicinal Chemistry Research
Year Published: 2020

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